KR20130002371A - Jak 억제제로서의 피라졸 유도체 - Google Patents
Jak 억제제로서의 피라졸 유도체 Download PDFInfo
- Publication number
- KR20130002371A KR20130002371A KR20127021643A KR20127021643A KR20130002371A KR 20130002371 A KR20130002371 A KR 20130002371A KR 20127021643 A KR20127021643 A KR 20127021643A KR 20127021643 A KR20127021643 A KR 20127021643A KR 20130002371 A KR20130002371 A KR 20130002371A
- Authority
- KR
- South Korea
- Prior art keywords
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- groups
- alkyl
- branched
- linear
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- 0 *c1c[n]2ncc(Br)c2c(*)n1 Chemical compound *c1c[n]2ncc(Br)c2c(*)n1 0.000 description 3
- LXFQSRIDYRFTJW-UHFFFAOYSA-M Cc(cc1C)cc(C)c1S([O-])(=O)=O Chemical compound Cc(cc1C)cc(C)c1S([O-])(=O)=O LXFQSRIDYRFTJW-UHFFFAOYSA-M 0.000 description 2
- JTAKTNUQPXTDBD-UHFFFAOYSA-N COc1ccnc(-c2c(cncc3)[n]3nc2)n1 Chemical compound COc1ccnc(-c2c(cncc3)[n]3nc2)n1 JTAKTNUQPXTDBD-UHFFFAOYSA-N 0.000 description 1
- YEUPWWFSFTVXRI-UHFFFAOYSA-N COc1ccnc(C#C)n1 Chemical compound COc1ccnc(C#C)n1 YEUPWWFSFTVXRI-UHFFFAOYSA-N 0.000 description 1
- YPCDTQRBGDJNAG-LBPRGKRZSA-N C[C@@H](c(nc1)ccc1F)Nc1nc(-c2c(cncc3)[n]3nc2)ncc1C Chemical compound C[C@@H](c(nc1)ccc1F)Nc1nc(-c2c(cncc3)[n]3nc2)ncc1C YPCDTQRBGDJNAG-LBPRGKRZSA-N 0.000 description 1
- ZKVNNWFQSWTQTA-ZDUSSCGKSA-N C[C@@H](c1ccccc1)Nc1nc(-c2c(cncc3)[n]3nc2)ncc1 Chemical compound C[C@@H](c1ccccc1)Nc1nc(-c2c(cncc3)[n]3nc2)ncc1 ZKVNNWFQSWTQTA-ZDUSSCGKSA-N 0.000 description 1
- CSYMZDKYDSLWGM-UHFFFAOYSA-N Cc(cc1C)cc(C)c1S(=O)=O Chemical compound Cc(cc1C)cc(C)c1S(=O)=O CSYMZDKYDSLWGM-UHFFFAOYSA-N 0.000 description 1
- CHKQALUEEULCPZ-UHFFFAOYSA-N Cc(cc1C)cc(C)c1S(ON)(=O)=O Chemical compound Cc(cc1C)cc(C)c1S(ON)(=O)=O CHKQALUEEULCPZ-UHFFFAOYSA-N 0.000 description 1
- AJRUTXNNHWTFCW-CQSZACIVSA-N Cc1cnc(-c2c(cncc3)[n]3nc2)nc1N[C@H](CCC1)CN1C(CC#N)=O Chemical compound Cc1cnc(-c2c(cncc3)[n]3nc2)nc1N[C@H](CCC1)CN1C(CC#N)=O AJRUTXNNHWTFCW-CQSZACIVSA-N 0.000 description 1
- HSWHRHVLLJLIDZ-UHFFFAOYSA-N Cc1cnc(-c2c(cncc3)[n]3nc2)nc1O Chemical compound Cc1cnc(-c2c(cncc3)[n]3nc2)nc1O HSWHRHVLLJLIDZ-UHFFFAOYSA-N 0.000 description 1
- JXEYLAJUOSDARA-UHFFFAOYSA-N Cc1cnc(-c2c(cncc3)[n]3nc2)nc1OC Chemical compound Cc1cnc(-c2c(cncc3)[n]3nc2)nc1OC JXEYLAJUOSDARA-UHFFFAOYSA-N 0.000 description 1
- ZVKCHNLTCSUIAJ-HDJSIYSDSA-N N#Cc(cc[n]1nc2)cc1c2-c1nc(N[C@H](CC2)CC[C@@H]2O)ccn1 Chemical compound N#Cc(cc[n]1nc2)cc1c2-c1nc(N[C@H](CC2)CC[C@@H]2O)ccn1 ZVKCHNLTCSUIAJ-HDJSIYSDSA-N 0.000 description 1
- OMYACPJCAZTMPH-NQPBPBACSA-N N=C/C(/c(nc1)nc(O)c1Cl)=C1\NC=CN=C1 Chemical compound N=C/C(/c(nc1)nc(O)c1Cl)=C1\NC=CN=C1 OMYACPJCAZTMPH-NQPBPBACSA-N 0.000 description 1
- LKCJATHTEIELPX-KLTOIVIWSA-N N=C/C(/c(nc1Cl)ncc1Cl)=C1\NC=CN=C1 Chemical compound N=C/C(/c(nc1Cl)ncc1Cl)=C1\NC=CN=C1 LKCJATHTEIELPX-KLTOIVIWSA-N 0.000 description 1
- XNDWREFVLHHENO-PHMKPSDGSA-N NN/C=C\N=C/C=[IH] Chemical compound NN/C=C\N=C/C=[IH] XNDWREFVLHHENO-PHMKPSDGSA-N 0.000 description 1
- OIQOROJAPKSOCE-UHFFFAOYSA-N N[n+]1ccncc1 Chemical compound N[n+]1ccncc1 OIQOROJAPKSOCE-UHFFFAOYSA-N 0.000 description 1
- STXDNNUBFOGQHA-UHFFFAOYSA-N Oc1ccnc(-c2c(cncc3)[n]3nc2)n1 Chemical compound Oc1ccnc(-c2c(cncc3)[n]3nc2)n1 STXDNNUBFOGQHA-UHFFFAOYSA-N 0.000 description 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N c1nccnc1 Chemical compound c1nccnc1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
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- A—HUMAN NECESSITIES
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- A61P11/02—Nasal agents, e.g. decongestants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P27/00—Drugs for disorders of the senses
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- A61P27/14—Decongestants or antiallergics
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- A—HUMAN NECESSITIES
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- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP10382039.5 | 2010-02-18 | ||
EP10382039A EP2360158A1 (en) | 2010-02-18 | 2010-02-18 | Pyrazole derivatives as jak inhibitors |
US30605110P | 2010-02-19 | 2010-02-19 | |
US61/306,051 | 2010-02-19 | ||
US37108110P | 2010-08-05 | 2010-08-05 | |
US61/371,081 | 2010-08-05 | ||
EP10382217.7 | 2010-08-05 | ||
EP10382217 | 2010-08-05 | ||
PCT/EP2011/000792 WO2011101161A1 (en) | 2010-02-18 | 2011-02-18 | Pyrazole derivatives as jak inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
KR20130002371A true KR20130002371A (ko) | 2013-01-08 |
Family
ID=43706312
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
KR20127021643A KR20130002371A (ko) | 2010-02-18 | 2011-02-18 | Jak 억제제로서의 피라졸 유도체 |
Country Status (21)
Country | Link |
---|---|
US (2) | US9206183B2 (es) |
EP (1) | EP2536728A1 (es) |
JP (1) | JP5820400B2 (es) |
KR (1) | KR20130002371A (es) |
CN (1) | CN102762570B (es) |
AR (1) | AR080187A1 (es) |
AU (1) | AU2011217489B2 (es) |
CA (1) | CA2790155A1 (es) |
CL (1) | CL2012002265A1 (es) |
CO (1) | CO6541658A2 (es) |
CR (1) | CR20120427A (es) |
EA (1) | EA201201143A1 (es) |
EC (1) | ECSP12012042A (es) |
GT (1) | GT201200243A (es) |
MX (1) | MX2012009430A (es) |
NZ (2) | NZ600881A (es) |
PE (1) | PE20130012A1 (es) |
SG (2) | SG182713A1 (es) |
UY (1) | UY33213A (es) |
WO (1) | WO2011101161A1 (es) |
ZA (1) | ZA201204959B (es) |
Families Citing this family (33)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
WO2012030918A1 (en) * | 2010-09-01 | 2012-03-08 | Ambit Biosciences Corporation | Adenosine a3 receptor modulating compounds and methods of use thereof |
EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
JP6105578B2 (ja) | 2011-07-21 | 2017-03-29 | トレロ ファーマシューティカルズ, インコーポレイテッド | 複素環式プロテインキナーゼ阻害剤 |
EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
LT2841428T (lt) | 2012-04-24 | 2018-12-10 | Vertex Pharmaceuticals Incorporated | Dnr-pk inhibitoriai |
US9013997B2 (en) | 2012-06-01 | 2015-04-21 | Broadcom Corporation | System for performing distributed data cut-through |
EA031405B1 (ru) | 2012-11-21 | 2018-12-28 | ПиТиСи ТЕРАПЬЮТИКС, ИНК. | Замещенные пиримидиновые обратные ингибиторы bmi-1 |
EP2938610A2 (en) * | 2012-12-28 | 2015-11-04 | The U.S.A. as represented by the Secretary, Department of Health and Human Services | Inhibitors of the usp1/uaf1 deubiquitinase complex and uses thereof |
AU2014205472B2 (en) | 2013-01-09 | 2018-05-10 | Concert Pharmaceuticals Inc. | Deuterated momelotinib |
EP3527563B1 (en) | 2013-03-12 | 2021-09-01 | Vertex Pharmaceuticals Incorporated | Dna-pk inhibitors |
EP3039015B1 (en) | 2013-08-30 | 2019-10-30 | PTC Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
CN105814036B (zh) | 2013-10-17 | 2018-10-26 | 沃泰克斯药物股份有限公司 | 作为dna-pk抑制剂的共晶 |
WO2015076800A1 (en) | 2013-11-21 | 2015-05-28 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine bmi-1 inhibitors |
BR112016012262B1 (pt) | 2013-12-05 | 2021-04-13 | Pfizer Inc | Acrilamidas heterocíclicas farmaceuticamente ativas e composições para tratar e prevenir condições mediadas por jac |
TW201605832A (zh) | 2013-12-10 | 2016-02-16 | 克立弗生物科學公司 | 作為p97錯合物之抑制劑之單環嘧啶/吡啶化合物 |
TW201605811A (zh) * | 2013-12-11 | 2016-02-16 | 阿爾米雷爾有限公司 | 作為jak抑制劑之吡唑并嘧啶-2基衍生物 |
EP3097092B1 (en) | 2014-01-20 | 2020-08-26 | Cleave Biosciences, Inc. | Fused pyrimidines as inhibitors of p97 complex |
EP3116506B1 (en) * | 2014-03-13 | 2019-04-17 | Merck Sharp & Dohme Corp. | 2-pyrazine carboxamides as spleen tyrosine kinase inhibitors |
TWI679205B (zh) | 2014-09-02 | 2019-12-11 | 日商日本新藥股份有限公司 | 吡唑并噻唑化合物及醫藥 |
KR20170090476A (ko) | 2014-12-05 | 2017-08-07 | 어레이 바이오파마 인크. | 야누스 키나제 저해제로서의 4,6-치환된-피라졸로[1,5-a]피라진 |
TW201705961A (zh) * | 2015-06-11 | 2017-02-16 | 阿爾米雷爾有限公司 | 作為jak抑制劑的2-(吡唑并吡啶-3-基)嘧啶衍生物 |
WO2017013270A1 (en) | 2015-07-23 | 2017-01-26 | Universite De Strasbourg | Use of leptin signaling inhibitor for protecting kidneys from patients having ciliopathy |
EA035036B1 (ru) * | 2016-02-24 | 2020-04-20 | Пфайзер Инк. | Производные пиразоло[1,5-а]пиразин-4-ила в качестве ингибиторов янус-киназы (jak) |
TWI712604B (zh) | 2016-03-01 | 2020-12-11 | 日商日本新藥股份有限公司 | 具jak抑制作用之化合物之結晶 |
KR20190062485A (ko) | 2016-09-27 | 2019-06-05 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-손상제 및 dna-pk 저해제의 조합을 사용한 암 치료 방법 |
WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | Pfizer Inc. | PYRAZOLO [1,5-A] PYRAZIN-4-YL AND RELATED DERIVATIVES |
CN112236139A (zh) | 2018-04-13 | 2021-01-15 | 大日本住友制药肿瘤公司 | 用于治疗骨髓增殖性肿瘤和与癌症相关的纤维化的pim激酶抑制剂 |
CA3109386A1 (en) | 2018-08-17 | 2020-03-19 | Ptc Therapeutics, Inc. | Use of 5-fluoro-2-(6-fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine in the treatment of pancreatic cancer |
WO2020092015A1 (en) | 2018-11-02 | 2020-05-07 | University Of Rochester | Therapeutic mitigation of epithelial infection |
WO2020167990A1 (en) | 2019-02-12 | 2020-08-20 | Tolero Pharmaceuticals, Inc. | Formulations comprising heterocyclic protein kinase inhibitors |
CN113924301B (zh) * | 2019-04-12 | 2024-08-16 | 北京普祺医药科技股份有限公司 | 一种吡唑并吡嗪衍生的化合物、药物组合物以及其用途 |
WO2024097653A1 (en) | 2022-10-31 | 2024-05-10 | Sumitomo Pharma America, Inc. | Pim1 inhibitor for treating myeloproliferative neoplasms |
Family Cites Families (50)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS54128591A (en) | 1978-03-25 | 1979-10-05 | Kyowa Hakko Kogyo Co Ltd | Cephalosporin analog |
CA2225396C (en) | 1995-06-21 | 2003-03-25 | Asta Medica Aktiengesellschaft | Pharmaceutical powder cartridge with integrated metering device and inhaler for powdered medicaments |
GB9919778D0 (en) * | 1999-08-21 | 1999-10-27 | Zeneca Ltd | Chemical compounds |
GB0020556D0 (en) * | 2000-08-22 | 2000-10-11 | Glaxo Group Ltd | Fused pyrazole derivatives |
PE20020506A1 (es) * | 2000-08-22 | 2002-07-09 | Glaxo Group Ltd | Derivados de pirazol fusionados como inhibidores de la proteina cinasa |
EP2048142A3 (en) | 2001-04-26 | 2009-04-22 | Eisai R&D Management Co., Ltd. | Nitrogen-containing condensed cyclic compound having a pyrazolyl group as a substituent group and pharmaceutical composition thereof |
DE10129703A1 (de) | 2001-06-22 | 2003-01-02 | Sofotec Gmbh & Co Kg | Zerstäubungssystem für eine Pulvermischung und Verfahren für Trockenpulverinhalatoren |
WO2003000682A1 (en) | 2001-06-25 | 2003-01-03 | Merck & Co., Inc. | (pyrimidyl)(phenyl)substituted fused heteroaryl p38 inhibiting and pkg kinase inhibiting compounds |
JP2005530745A (ja) | 2002-05-02 | 2005-10-13 | メルク エンド カムパニー インコーポレーテッド | チロシンキナーゼ阻害剤 |
ES2195785B1 (es) | 2002-05-16 | 2005-03-16 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
EP1507779A1 (en) * | 2002-05-30 | 2005-02-23 | Vertex Pharmaceuticals Incorporated | Inhibitors of jak and cdk2 protein kinases |
ES2211344B1 (es) | 2002-12-26 | 2005-10-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
ES2232306B1 (es) | 2003-11-10 | 2006-08-01 | Almirall Prodesfarma, S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
KR101216372B1 (ko) * | 2004-03-30 | 2013-01-04 | 버텍스 파마슈티칼스 인코포레이티드 | Jak 및 기타 단백질 키나제의 억제제로서 유용한 아자인돌 |
ES2251866B1 (es) | 2004-06-18 | 2007-06-16 | Laboratorios Almirall S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
ES2251867B1 (es) | 2004-06-21 | 2007-06-16 | Laboratorios Almirall S.A. | Nuevos derivados de piridazin-3(2h)-ona. |
WO2006008207A1 (de) | 2004-07-17 | 2006-01-26 | Robert Bosch Gmbh | Sigma-delta-modulator |
WO2006038001A1 (en) | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
JP5132319B2 (ja) * | 2004-12-21 | 2013-01-30 | スミスクライン ビーチャム コーポレーション | 2−ピリミジニルピラゾロピリジンErbBキナーゼ阻害剤 |
ES2555063T3 (es) | 2005-02-04 | 2015-12-28 | Astrazeneca Ab | Derivados de pirazolilaminopiridina útiles como inhibidores de quinasas |
ES2265276B1 (es) | 2005-05-20 | 2008-02-01 | Laboratorios Almirall S.A. | Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico. |
ES2296516B1 (es) | 2006-04-27 | 2009-04-01 | Laboratorios Almirall S.A. | Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico. |
EP2038279A2 (en) * | 2006-06-06 | 2009-03-25 | Avigen, Inc. | Substituted pyrazolo [1,5- alpha] pyridine compounds and their methods of use |
AR063142A1 (es) | 2006-10-04 | 2008-12-30 | Pharmacopeia Inc | Derivados de 2-(bencimidazolil) purina y purinonas 6-sustituidas utiles como inmunosupresores,y composiciones farmaceuticas que los contienen. |
AU2007307031B2 (en) | 2006-10-11 | 2011-11-24 | Amgen Inc. | Imidazo- and triazolo-pyridine compounds and methods of use therof |
ES2302447B1 (es) | 2006-10-20 | 2009-06-12 | Laboratorios Almirall S.A. | Derivados de 4-(2-amino-1-hidroxietil)fenol como agonistas del receptor beta2 adrenergico. |
ES2319596B1 (es) | 2006-12-22 | 2010-02-08 | Laboratorios Almirall S.A. | Nuevos derivados de los acidos amino-nicotinico y amino-isonicotinico. |
EP2121687B1 (en) * | 2006-12-22 | 2015-10-14 | Astex Therapeutics Limited | Tricyclic amine derivatives as protein tyrosine kinase inhibitors |
US7977336B2 (en) | 2006-12-28 | 2011-07-12 | Banyu Pharmaceutical Co. Ltd | Aminopyrimidine derivatives as PLK1 inhibitors |
ES2306595B1 (es) | 2007-02-09 | 2009-09-11 | Laboratorios Almirall S.A. | Sal de napadisilato de 5-(2-((6-(2,2-difluoro-2-feniletoxi)hexil)amino)-1-hidroxietil)-8-hidroxiquinolin-2(1h)-ona como agonista del receptor adrenergico beta2. |
US7834024B2 (en) | 2007-03-26 | 2010-11-16 | Rigel Pharmaceuticals, Inc. | Compositions and methods for inhibition of the JAK pathway |
KR20100032886A (ko) * | 2007-06-08 | 2010-03-26 | 아보트 러보러터리즈 | 키나제 억제제로서의 5-헤테로아릴 치환된 인다졸 |
UY31272A1 (es) | 2007-08-10 | 2009-01-30 | Almirall Lab | Nuevos derivados de ácido azabifenilaminobenzoico |
ATE503757T1 (de) | 2007-08-14 | 2011-04-15 | Bayer Schering Pharma Ag | Kondensierte imidazole zur krebsbehandlung |
WO2009026254A1 (en) | 2007-08-17 | 2009-02-26 | Icagen, Inc. | Heterocycles as potassium channel modulators |
CA2703037A1 (en) | 2007-10-17 | 2009-04-23 | Novartis Ag | Organic compounds |
CA2703125C (en) * | 2007-10-25 | 2012-08-28 | David J. Guerin | Pyrazinyl-substituted pyrrolo[2,3-b]pyridines, compositions thereof, and their use in the treatment of cancer |
AU2008343173A1 (en) | 2007-12-19 | 2009-07-09 | Aj Park | Pyrazolo [1,5-a] pyrimidines useful as JAK2 inhibitors |
AU2008345681A1 (en) | 2007-12-21 | 2009-07-09 | Wyeth Llc | Imidazo [1,2-a] pyridine compounds |
AU2009218607B2 (en) | 2008-02-25 | 2014-02-13 | F. Hoffmann-La Roche Ag | Pyrrolopyrazine kinase inhibitors |
WO2010016005A1 (en) * | 2008-08-06 | 2010-02-11 | Pfizer Inc. | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
TW201022262A (en) | 2008-10-29 | 2010-06-16 | Astrazeneca Ab | Novel compounds 515 |
AR074870A1 (es) * | 2008-12-24 | 2011-02-16 | Palau Pharma Sa | Derivados de pirazolo (1,5-a ) piridina |
UA109775C2 (xx) | 2009-10-29 | 2015-10-12 | N-вмісні гетероарильні похідні як інгібітори jak3-кінази | |
EP2338888A1 (en) | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
EP2397482A1 (en) | 2010-06-15 | 2011-12-21 | Almirall, S.A. | Heteroaryl imidazolone derivatives as jak inhibitors |
EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
EP2527344A1 (en) | 2011-05-25 | 2012-11-28 | Almirall, S.A. | Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases |
EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
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- 2011-02-18 NZ NZ60088111A patent/NZ600881A/en not_active IP Right Cessation
- 2011-02-18 EP EP11704553A patent/EP2536728A1/en not_active Withdrawn
- 2011-02-18 PE PE2012001249A patent/PE20130012A1/es not_active Application Discontinuation
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- 2011-02-18 CA CA 2790155 patent/CA2790155A1/en not_active Abandoned
- 2011-02-18 US US13/579,344 patent/US9206183B2/en not_active Expired - Fee Related
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CO6541658A2 (es) | 2012-10-16 |
US20130209400A1 (en) | 2013-08-15 |
US20140086870A9 (en) | 2014-03-27 |
CL2012002265A1 (es) | 2013-02-15 |
GT201200243A (es) | 2015-06-02 |
AU2011217489A1 (en) | 2012-08-30 |
EA201201143A1 (ru) | 2013-03-29 |
CA2790155A1 (en) | 2011-08-25 |
SG182713A1 (en) | 2012-09-27 |
MX2012009430A (es) | 2012-09-07 |
CN102762570A (zh) | 2012-10-31 |
PE20130012A1 (es) | 2013-01-28 |
US9206183B2 (en) | 2015-12-08 |
CN102762570B (zh) | 2015-11-25 |
JP2013519696A (ja) | 2013-05-30 |
NZ600881A (en) | 2014-12-24 |
US20150118186A1 (en) | 2015-04-30 |
WO2011101161A1 (en) | 2011-08-25 |
JP5820400B2 (ja) | 2015-11-24 |
ECSP12012042A (es) | 2013-05-31 |
NZ701440A (en) | 2015-05-29 |
CR20120427A (es) | 2013-01-30 |
SG10201500735VA (en) | 2015-04-29 |
EP2536728A1 (en) | 2012-12-26 |
AU2011217489B2 (en) | 2015-09-03 |
AR080187A1 (es) | 2012-03-21 |
UY33213A (es) | 2011-09-30 |
ZA201204959B (en) | 2013-03-27 |
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